A fixed-dose combination (FDC) oral anti-diabetic drug containing a third-generation sulfonylurea (Glimepiride) and a biguanide (Metformin). It is indicated for the management of type 2 diabetes mellitus in patients inadequately controlled on diet and exercise plus either metformin or a sulfonylurea alone. This combination provides synergistic action by increasing insulin secretion (Glimepiride) and decreasing hepatic glucose production and improving insulin sensitivity (Metformin).
Adult: Usual starting dose: One tablet (Glimepiride 1mg + Metformin 500mg) once or twice daily with meals. Dose must be individualized based on glycemic response. Maximum recommended daily dose: Glimepiride 8mg + Metformin 2000mg. The dose of Metformin should be titrated slowly to minimize GI side effects.
Note: Administer with or immediately after the main meals (breakfast and/or dinner) to reduce the gastrointestinal side effects of Metformin. Tablet should be swallowed whole with a glass of water; do not crush or chew.
The combination works via complementary mechanisms to lower blood glucose. Glimepiride stimulates insulin release from pancreatic beta-cells by binding to sulfonylurea receptors (SUR1) on ATP-sensitive potassium channels, leading to membrane depolarization and calcium influx. Metformin decreases hepatic gluconeogenesis, increases peripheral glucose uptake and utilization (improves insulin sensitivity), and decreases intestinal absorption of glucose.
Pregnancy: Category C (US FDA). Not recommended during pregnancy. Insulin is the drug of choice for controlling diabetes in pregnant women. Both drugs cross the placenta. Metformin may be used in gestational diabetes under specialist supervision, but this FDC is not recommended.
Driving: Caution advised. The drug can cause hypoglycemia or dizziness, which may impair the ability to concentrate and react. Patients should be aware of hypoglycemia symptoms, especially when driving.
| Other Hypoglycemic Agents (Insulin, Thiazolidinediones) | Increased risk of hypoglycemia. | Major |
| Beta-blockers (e.g., Propranolol) | May potentiate hypoglycemia and mask its adrenergic warning signs (tachycardia). | Moderate |
| Alcohol | Acute: Increases risk of hypoglycemia. Chronic: Increases risk of lactic acidosis with Metformin. | Major |
| Warfarin | Sulfonylureas may potentiate anticoagulant effect. | Moderate |
| CYP2C9 Inhibitors (e.g., Fluconazole, Amiodarone) | Increase Glimepiride plasma levels, risk of hypoglycemia. | Moderate |
| CYP2C9 Inducers (e.g., Rifampicin) | Decrease Glimepiride plasma levels, reducing efficacy. | Moderate |
| Cationic Drugs (e.g., Cimetidine, Ranitidine, Digoxin, Morphine, Vancomycin) | Competitively inhibit renal tubular secretion of Metformin, potentially increasing its levels. | Moderate |
| Diuretics (especially Thiazides) | May cause hyperglycemia, reducing efficacy. | Moderate |
| Corticosteroids (e.g., Prednisolone) | Cause hyperglycemia, reducing efficacy. | Major |
| Iodinated Contrast Media | Risk of lactic acidosis. Metformin must be withheld before and after procedure. | Major |
Same composition (Glimepiride (1mg) + Metformin (500mg)), different brands: